Tag: M.W=150-200

Bos, Pieter H. published the artcileDevelopment of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents, Formula: C7H10BNO3, the publication is Cell Chemical Biology (2019), 26(12), 1703-1715.e37, database is CAplus and MEDLINE.

Disease-causing mutations in many neurodegenerative disorders lead to proteinopathies that trigger endoplasmic reticulum (ER) stress. However, few therapeutic options exist for patients with these diseases. Using an in vitro screening platform to identify compounds that protect human motor neurons from ER stress-mediated degeneration, we discovered that compounds targeting the mitogen-activated protein kinase kinase kinase kinase (MAP4K) family are neuroprotective. The kinase inhibitor URMC-099 (compound 1) stood out as a promising lead compound for further optimization. We coupled structure-based compound design with functional activity testing in neurons subjected to ER stress to develop a series of analogs with improved MAP4K inhibition and concomitant increases in potency and efficacy. Further structural modifications were performed to enhance the pharmacokinetic profiles of the compound 1 derivatives Prostetin/12k emerged as an exceptionally potent, metabolically stable, and blood-brain barrier-penetrant compound that is well suited for future testing in animal models of neurodegeneration.

Cell Chemical Biology published new progress about 612845-44-0. 612845-44-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Boronic Acids,Boronic acid and ester, name is (6-Ethoxypyridin-3-yl)boronic acid, and the molecular formula is C7H10BNO3, Formula: C7H10BNO3.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Ishida, Yoshiyuki published the artcileSequence selective dual-emission detection of (i, i + 1) bis-phosphorylated peptide using diazastilbene-type Zn(ii)-Dpa chemosensor, COA of Formula: C7H6ClNO2, the main research area is sequence selective dual emission bisphosphorylated peptide diazastilbene zinc chemosensor.

This paper describes a new fluorescent chemosensor for phosphorylated peptide, which comprises a rigid trans-4,4′-diazastilbene and two Zn(II)-Dpa (2,2′-dipicolylamine) units; this chemosensor sequence-selectively binds to a (i, i + 1) bis-phosphorylated peptide and displays a dual-emission fluorescence change.

Chemical Communications (Cambridge, United Kingdom) published new progress about Affinity. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, COA of Formula: C7H6ClNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ashworth, Ian W. published the artcileProcess Development of a Suzuki Reaction Used in the Manufacture of Lanabecestat, HPLC of Formula: 917471-30-8, the main research area is lanabecestat preparation; Suzuki coupling diethanolamine alkynylpyridinylboronate bromodispirocyclohexaneindaneimidazole key step; hydrolysis kinetics diethanolamine alkynylpyridinylboronate; effect diethanolamine removal palladium lanabecestat.

A process for preparation of the potential anti-Alzheimer’s agent lanabecestat was developed by coupling of an alkynylpyridinylboronic acid diethanolamine ester with a bromodispirocyclohexaneindaneimidazole in the presence of Pd(AmPhos)2Cl2 and K3PO4 in EtOH/H2O; the new process reduced the need for solvent changes and difficult isolation steps and decreased the amount of palladium detected in the final product without the use of solid-phase extractants. The kinetics of hydrolysis of the diethanolamine boronate and the free boronic acid was determined; diethanolamine generated in the hydrolysis decreased the rate of coupling but likely improved the purge of palladium from the product.

Organic Process Research & Development published new progress about Hydrolysis. 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, HPLC of Formula: 917471-30-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Puszko, A. published the artcile13C NMR spectra of 2,4-dihalopicolines and their N-oxides and IR spectra of 2-halopicoline N-oxides, 2,4-dihalopicoline N-oxides and 2-halo-4-nitropicoline N-oxides, Safety of 2,4-Dichloro-3-methylpyridine, the main research area is NMR IR spectra halopicoline; picoline halo NMR IR spectra; substituent effect NMR IR spectra halopicoline.

The 13C NMR and IR spectra of the title compounds were recorded and their spectral parameters assigned. The influence of electronic properties of the substituents on the direction of chem. shifts and νN-O values is discussed. The ratio between a substituted heterocyclic compound and its parent and the identically substituted benzene derivatives has been determined

Polish Journal of Chemistry published new progress about IR spectra. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Safety of 2,4-Dichloro-3-methylpyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Maiden, Tracy M. M. published the artcileSynthesis of Functionalized Pyridines via a Regioselective Oxazoline Promoted C-H Amidation Reaction, Recommanded Product: Ethyl 6-chloropicolinate, the main research area is oxazolylpyridine functionalized preparation rhodium silver catalyzed amidation; azaquinazoline scaffold preparation; pyridopyrimidinone preparation; nicotinamide derivative preparation heterocyclization; picolinamide derivative preparation heterocyclization.

The 1st Rh-catalyzed C-H amidation of pyridines is reported. The incorporation of a substituent at the C2 position both is crucial to the success of this transformation and provides considerable scope for further elaboration of the resulting products. Among these compounds, 2-chloropyridines allow access to a selection of intermediates including a versatile azaquinazoline scaffold.

Organic Letters published new progress about Amidation. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, Recommanded Product: Ethyl 6-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Young, Ian S. published the artcilePalladium-Catalyzed Site-Selective Amidation of Dichloroazines, Synthetic Route of 132097-09-7, the main research area is dichloroazine amide amidation palladium; chloroazinyl amide regioselective preparation; palladium amidation catalyst.

A highly site-selective amidation reaction of substituted 2,4-dichloroazines is reported. Palladium acetate/1,1′-bis(diphenylphosphino)ferrocene (dppf) was identified as the optimal catalyst system, producing >99:1 C-2/C-4 selectivity for most examples. The generality of this transformation was demonstrated through a survey of a diverse amide/substituted 2,4-dichloroazine scope, leading to the preparation of the desired C-2 amidated products in good to excellent yields.

Organic Letters published new progress about Amidation. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Synthetic Route of 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mayer, Joachim M. published the artcileDeviations in the log P (partition coefficient) of protonated arylalkylamines and in their apparent log P, COA of Formula: C7H11ClN2, the main research area is amine aryl protonated partition coefficient; pyridylamine partition coefficient; phenylalkylamine partition coefficient.

Partition coefficients of monoprotonated phenyl- and 2-, 3-, and 4-pyridyl-substituted alkylamines show unpredictable but consistent trends. The coefficients of the Me, Bu, and pentyl homologs in each series are linearly related, while the Et and Pr derivatives appear too lipophilic. Thus, these partition coefficients are affected by perturbative effects, e.g., hydration or ion pairing. Also, the phosphate buffers yield abnormally low partition coefficient values.

European Journal of Medicinal Chemistry published new progress about Additivity. 84359-16-0 belongs to class pyridine-derivatives, name is 2-(Pyridin-3-yl)ethanamine hydrochloride, and the molecular formula is C7H11ClN2, COA of Formula: C7H11ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Young, Summer E. published the artcileSynthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets, SDS of cas: 321438-86-2, the main research area is proteinase activated receptor PAR4.

Protease activated receptor-4 [PAR4, proteinase-activated receptor PAR-4] is one of thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. The authors sought to develop potent, selective and novel PAR4 antagonists to test the role of PAR4 in thrombosis and hemostasis. The development of an expedient three-step synthetic route to access a novel series of indole-based PAR4 antagonists also necessitated the development of a platelet based high-throughput screening assay. Screening and subsequent structure activity relationship anal. yielded several selective PAR4 antagonists as well as possible new scaffolds for future antagonist development. The title compounds thus formed included an indole benzoic acid ester (I) and related substances. I was evaluated against an indazole benzoic acid ester analog (II) [i.e., 4-[1-(phenylmethyl)-1H-indazol-3-yl]benzoic acid Et ester]. The synthesis of the target compounds was achieved using 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole as starting materials. The synthetic sequence involved an alkylation of 1H-pyrrolo[2,3-b]pyridine, 1H-indole and 1H-indazole, formation of bromide derivatives and a subsequent coupling reaction with boronic acids.

PLoS One published new progress about Allosterism. 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, SDS of cas: 321438-86-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Puszko, A. published the artcileElectric dipole moments of 2,4-dihalopicolines and their N-oxides, Application In Synthesis of 132097-09-7, the main research area is dipole moment picoline oxide halogen derivative.

Dipole moment values of 2,4-dichloro- and 2,4-dibromopicolines and their N-oxides were calculated from the permittivity and refractive indexes measurements as well as by means of composition of groups and bonds moments vectors. The influence of substituents effects on the dipole moment values was discussed and the results obtained were compared.

Chemical Papers published new progress about Dipole moment. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Application In Synthesis of 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bach, Peter published the artcileEffects of the Pyridine 3-Substituent on Regioselectivity in the Nucleophilic Aromatic Substitution Reaction of 3-Substituted 2,6-Dichloropyridines with 1-Methylpiperazine Studied by a Chemical Design Strategy, SDS of cas: 132097-09-7, the main research area is effect dichloropyridine substituent regioselectivity nucleophilic aromatic substitution reaction.

A chem. design strategy has been used to select 3-substituted 2,6-dichloropyridines for the nucleophilic aromatic substitution reaction with 1-methylpiperazine. The aim was to study the dependency of the regioselectivity in these reactions on the character of the pyridine 3-substituent expressed by their lipophilicity (PI), size (MR), and inductive effect (σp). Interestingly, the regioselectivity did not correlate with any of these parameters, but in a statistically significant manner with the Verloop steric parameter B1, as indicated by the p value of 0.006 (R2 = 0.45). This implies that bulky 3-substituents close to the pyridine ring induce regioselectivity towards the 6-position. Useful in practical synthesis is the different regioselectivity obtained with a carboxylic acid 3-substituent and precursors or derivatives thereof. Thus, in acetonitrile as solvent, 3-carboxylate and 3-amide substituents were preferred to obtain the 2-isomer (9:1 ratio of the 6-isomer), whereas the 3-cyano and 3-trifluoromethyl substituents were preferred to obtain the 6-isomer (9:1 ratio of the 2-isomer). Anal. of the regioselectivity Rsel for the pyridine 2-position in the reaction of 2,6-dichloro-3-(methoxycarbonyl)pyridine with 1-methylpiperazine in 21 different solvents showed that Rsel could be predicted by the Kamlet-Taft equation: Rsel = 1.28990 + 0.03992α – 0.59417β – 0.46169π* (R2 = 0.95, p = 1.9 × 10-10). Rsel is thus mainly correlated with the ability of the solvent to function as a hydrogen-bond acceptor, as expressed by the solvatochromic β parameter. Thus, the 16:1 regioselectivity for the 2-isomer in DCM (β = 0.10) could be switched to a 2:1 selectivity for the 6-isomer in DMSO (β = 0.76).

European Journal of Organic Chemistry published new progress about Hydrogen bond. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, SDS of cas: 132097-09-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem